全部商品分类首页
TAK-715
.jpg)
1/2
用小程序，查商品更便捷
产品介绍
产品介绍
产品信息
抗原名称
p38α ,p38β
商品描述
TAK-715是一种p38 MAPK抑制剂，作用于p38α，IC50为7.1 nM，作用于p38α比作用于p38β选择性高28倍多，对p38γ/δ， JNK1， ERK1， IKKβ， MEKK1和TAK1没有抑制作用。TAK 715抑制LPS刺激的TNF-α从THP-1释放，IC50为48 nM。 TAK 715 (10 μM)作用于U2OS-EFC细胞，抑制Wnt-3a诱导的hDvl2磷酸化和hDvl2转变。 TAK715的酰胺NH通过氢键结合到p38α的Met109的主链羰基上。
分子量
399.51
纯度
>98%
可溶性
Ethanol ：20 mg/mL (50 mM)
DMSO ：40 mg/mL (100 mM)
DMSO ：40 mg/mL (100 mM)
外观
白色固体
In vitro(体外研究)
TAK 715 inhibits LPS-stimulated release of TNF-alpha from THP-1 with IC50 of 48 nM. TAK 715 (10 μM) inhibits Wnt-3a-induced hDvl2 phosphorylation and the hDvl2 shift in U2OS-EFC cells. The amide NH of TAK 715 is hydrogen bonded to the main-chain carbonyl of Met109 of p38 alpha. TAK 715 binds relatively high in the ATP pocket, occupying the hydrophobic back pocket, the adenine region and the front pocket of p38 as well as extending to most of the length of the Gly-rich loop.
In vivo(体内研究)
TAK 715 (10 mg/kg, po) inhibits LPS-induced TNF-alpha production in mice with 87.6% inhibition. TAK 715 has a modest mouse bioavailability of 18.4% and a slightly improved rat bioavailability of 21.1%. TAK 715 has a modest mouse bioavailability of 18.4% and a slightly improved rat bioavailability of 21.1%. TAK 715 results in Cmax of 0.19 μg/mL and AUC(0-24 hours) of 1.16 μg·h/mL in rats. TAK 715 (30 mg/kg, po) significantly reduces the secondary paw volume with 25 % inhibition in a rat adjuvant-induced arthritis (AA) model.
背景
别名
N-(4-(2-乙基-4-(3-甲基苯基)噻唑-5-基)吡啶-2-基)苯甲酰胺
分子式
C24H21N3OS
CAS号
303162-79-0
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
声明 ：本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。